کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1360503 | 981438 | 2008 | 7 صفحه PDF | دانلود رایگان |
Series of curcumin derivatives were synthesized; the inhibitory activities on thioredoxin reductase (TrxR) of all analogues were evaluated by DTNB assay in vitro. It is found that most of the analogues can inhibit TrxR in the low micromolar range; Structure-activity relationship analysis reveals that analogues with furan moiety have excellent inhibitory effect on TrxR in an irreversible manner, indicating that the furan moiety may serve as a possible pharmacophore during the interaction of curcumin analogues with TrxR. The effect of selected curcuminoids on growth of different TrxR overexpressed cancer cell lines was also investigated and discussed.
Series of curcumin derivatives were synthesized and evaluated for the inhibitory activities on TrxR by DTNB assay; it is found that most of the analogues can inhibit TrxR in vitro; SAR analysis reveals that analogues with furan moiety have excellent inhibitory effect on TrxR.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry - Volume 16, Issue 17, 1 September 2008, Pages 8035–8041